A novel 5-HT2A receptor antagonist exhibits antidepressant-like effects in a battery of rodent behavioural assays: Approaching early-onset antidepressants

Pharmacology Biochemistry and Behavior

Volumn 94, Issue 3, 2010, Pages 363-373

  Pandey, Dilip Kumar ^a   Mahesh, Radhakrishnan ^a   kumar, Akutota Ashok ^a   Rao, V Sambasiva ^a   Arjun, Muralidharan ^a   Rajkumar, Ramamoorthy ^a  

^a BIRLA INSTITUTE OF TECHNOLOGY AND SCIENCE   (India)

Author keywords

5 HT2A receptor antagonist; Antidepressant test battery; Depression; Early onset; Mice; Olfactory bulbectomy; Rat

Indexed keywords

(3 CHLOROPHENYL)PIPERAZINE; 5 [[4 BENZO[ALPHA]ISOTHIAZOL 3 YL]PIPERAZIN 1 YL]METHYL 6 CHLOROINDOLIN 2 ONE; AMITRIPTYLINE; ANTIDEPRESSANT AGENT; FLUOXETINE; HARMAN; KETANSERIN; PAROXETINE; QUIPAZINE; SEROTONIN 2A ANTAGONIST; SEROTONIN 2A RECEPTOR; SUCROSE; TRICYCLIC ANTIDEPRESSANT AGENT; UNCLASSIFIED DRUG; VENLAFAXINE;

ANIMAL BEHAVIOR; ANIMAL EXPERIMENT; ANTIDEPRESSANT ACTIVITY; ARTICLE; CONTROLLED STUDY; DEPRESSION; DRUG ACTIVITY; EMOTIONALITY; FOOD PREFERENCE; FORCED SWIMMING TEST; HEAD TWITCH; LONG TERM CARE; MALE; MOUSE; NONHUMAN; OLFACTORY BULBECTOMY; OPEN FIELD BEHAVIOR; PRIORITY JOURNAL; RAT; RECEPTOR AFFINITY; RODENT; SHORT COURSE THERAPY; SOCIAL INTERACTION;

ANIMALS; ANTIDEPRESSIVE AGENTS, SECOND-GENERATION; BEHAVIOR, ANIMAL; DOSE-RESPONSE RELATIONSHIP, DRUG; INDOLES; MALE; MICE; QUIPAZINE; RATS; RATS, WISTAR; RECEPTOR, SEROTONIN, 5-HT2A; SEROTONIN ANTAGONISTS; THIAZOLES;

MUS; RATTUS; RODENTIA;

EID: 72149119722     PISSN: 00913057     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.pbb.2009.09.018     Document Type: Article

References (115)

1. Adell A., Castro E., Celada P., Bortolozzi A., Pazos A., and Artigas F. Strategies for producing faster acting antidepressants. Drug Discov Today 10 (2005) 578-585
2. Anand A., Charney D.S., Delgado P.L., Mc Dougle C.J., Heninger G.R., and Price L.H. Neuroendocrine and behavioural responses to intravenous m-chlorophenylpiprazine (mCPP) in depressed patient and healthy comparison subjects. Am J Psychiatry 151 (1994) 1626-1627
3. Anttila S.A.K., and Leinonen E.V.J. A review of the pharmacological and clinical profile of mirtazapine. CNS Drug Rev 7 (2001) 249-264
4. 2 and beta-adrenergic receptor binding in the brain of suicide victims. Arch Gen Psychiatry 47 (1990) 1038-1047
5. 2 binding sites in frontal cortex of suicide victims and control subjects. Am J Psychiatry 146 (1989) 730-736
6. Artigas F. Limitations to enhancing the speed of onset of antidepressants-are rapid action antidepressants possible?. Hum Psychopharmacol 16 (2001) 29-36
7. Basso A.M., Gallagher K.B., Bratcher N.A., Brioni J.D., Moreland R.B., Hsieh G.C., et al. Antidepressant-like effect of D(2/3) receptor-, but not D(4) receptor-activation in the rat forced swim test. Neuropsychopharmacology 30 (2005) 1257-1268
8. Blackshear M.A., and Sanders-Bush E. Serotonin receptor sensitivity after acute and chronic treatment with mianserin. J Pharmacol Exp Ther 221 (1982) 303-308
9. Blier P. The pharmacology of putative early-onset antidepressant strategies. Eur Neuropsychopharmacology 13 (2003) 57-66
10. Boissier J.R., and Simon P. Action of caffeine on the spontaneous motility of the mouse. Arch Int Pharmacodyn Ther 158 (1965) 212-222
11. Borsini F., Cesana R., Kelly J., Leonard B.E., McNamara M., Richards J., et al. BIMT 17: a putative antidepressant with a fast onset of action?. Psychopharmacology (Berl) 134 (1997) 378-386
12. Borsini F., Evans K., Jason K., Rohde F., Alexander B., and Pollentier S. Pharmacology of flibanserin. CNS Drug Rev 8 (2002) 117-142
13. Bourin M., Hascoët M., Colombel M.C., Coutts R.T., and Baker G.B. Clonidine potentiates the effects of tranylcypromine, phenelzine and two analogues in the forced swimming test in mice. J Psychiatry Neurosci 27 (2002) 178-185
14. 2 receptors. Behav Pharmacol 17 (2006) 559-572
15. Butler J., and Leonard B.E. The platelet serotonergic system in depression and following sertraline treatment. Int Clin Psychopharmacol 3 (1988) 343-347
16. Cairncross K.D., Cox B., Forster C., and Wren A.F. Olfactory projection systems, drugs and behavior: a review. Psychoneuroendocrinology 4 (1979) 253-272
17. 2A receptors in depression. J Psychiatry Neurosci 29 (2004) 252-265
18. 2 binding site changes. Br J Pharmacol 93 (1988) 331-336
19. Cryan J.F., Mc Grath C., Leonard B.E., and Norman T.R. Combining pindolol and paroxetine in an animal model of chronic anti depressant action. Can early onset of action be detected?. Eur J Pharmacol 352 (1998) 23-28
20. Darmani N.A., and Gerdes C.F. Temporal differential adaptation of head-twitch and ear-scratch responses following administration of challenge doses of DOI. Pharmacol Biochem Behav 50 (1995) 545-550
21. Davis R., Whittington R., and Bryson H.M. Nefazodone. A review of its pharmacology and clinical efficacy in the management of major depression. Drugs 53 (1997) 608-636
22. Derivan A.T. Antidepressants: can we determine how quickly they work? Issues from the literature. Psychopharmacol Bull 31 (1995) 23-28
23. Dremencov E., Gispan-Herman I., Rosenstein M., Mendelman A., Overstreet D.H., Zohar J., et al. The serotonin-dopamine interaction is critical for fast-onset action of antidepressant treatment: in vivo studies in an animal model of depression. Prog Neuropsychopharmacol Biol Psychiatry 28 (2004) 141-147
24. Dursun S.M., Bird D., and Ronson K.E. Nefazodone treatment of dysthymic disorder an open, long-term, prospective pilot study. Prog Neuropsychopharmacol Biol Psychiatry 26 (2002) 671-676
25. 2 receptors in olfactory bulbectomised (OB) rats after chronic treatment with mianserin and desipramine. Hum. Psychopharmacol (Berl) 9 (1994) 397-407
26. El Mansari M., and Blier P. In vivo electrophysiological assessment of the putative antidepressant Wf-516 in the rat raphe dorsalis, locus coeruleus and hippocampus. Naunyn Schmiedebergs Arch Pharmacol 376 (2008) 351-361
27. Farzin D., and Mansouri N. Antidepressant-like effect of harmane and other beta-carbolines in the mouse forced swim test. Eur Neuropsychopharmacol 16 (2006) 324-328
28. Fawcett J., and Barkin R.L. Review of the results from clinical studies on the efficacy, safety and tolerability of mirtazapine for the treatment of patients with major depression. J Affect Disord 51 (1998) 267-285
29. File S.E., and Hyde J.R. Can social interaction be used to measure anxiety?. Br J Pharmacol 62 (1978) 19-24
30. Gelenberg A.J., and Chesen C.L. How fast are antidepressants?. J Clin Psychiatry 61 (2000) 712-721
31. Gelenberg A.J., Trivedi M.H., Rush A.J., Thase M.E., Howland R., Klein D.N., et al. Randomized, placebo-controlled trial of nefazodone maintenance treatment in preventing recurrence in chronic depression. Biol Psychiatry 54 (2003) 806-817
32. Gobert A., and Millan M.J. Serotonin (5-HT)2A receptor activation enhances dialysate levels of dopamine and noradrenaline, but not 5-HT, in the frontal cortex of freely-moving rats. Neuropharmacology 38 (1999) 315-317
33. 2 receptor-mediated head-twitch behavior following antidepressant treatment to mice. Br J Pharmacol 83 (1984) 235-242
34. Gray J.A., and Roth B.L. Paradoxical trafficking and regulation of 5-HT(2A) receptors by agonists and antagonists. Brain Res Bull 56 (2001) 441-451
35. Grecksch G., Zhou D., and Franke C. Influence of olfactory bulbectomy and subsequent imipramine treatment on serotonin presynapses in the rat frontal cortex. Br J Pharmacol 122 (1997) 1725-1731
36. 2 receptor number in frontal cortex. Br J Pharmacol 80 (1983) 377-385
37. 1A receptors in mice. Pharmacol Biochem Behav 45 (1993) 65-70
38. Hanley N.R., and Hensler J.G. Mechanisms of ligand-induced desensitization of the 5-hydroxytryptamine(2A) receptor. J Pharmacol Exp Ther 300 (2002) 468-477
39. Harkin A., Kelly J.P., and Leonard B.E. A review of the relevance and validity of olfactory bulbectomy as a model of depression. Clin Neurosci Res 3 (2003) 253-262
40. Howard H.R., Lowe III J.A., Seeger T.F., Seymour P.A., Zorn S.H., Maloney P.R., et al. 3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents. J Med Chem 39 (1996) 143-148
41. Huang M., Ichiwaka J., Li Z., Dai J., and Meltzer H.Y. Augmentation by citalopram of risperidone-induced monoamine release in rat prefrontal cortex. Psychopharmacology (Berl) 185 (2006) 274-281
42. Kelly J.P., Wyrnn A.S., and Leonard B.E. Olfactory bulbectomized rat as a model of depression: an update. Pharmcol Ther 74 (1997) 299-316
43. Lumia A.R., Teicher M.H., Salchli F., Ayers E., and Possidente B. Olfactory bulbectomy as a model for agitated hyposerotonergic depression. Brain Res 587 (1992) 181-185
44. 1A receptors. Br J Pharmacol 108 (1993) 669-677
45. Machado-Vieira R., Salvadore G., Luckenbaugh D.A., Manji H.K., and Zarate Jr. C.A. Rapid onset of antidepressant action: a new paradigm in the research and treatment of major depressive disorder. J Clin Psychiatry 69 (2008) 946-958
46. Macs M., Vandoolaeghe E., and Desnyder R. Efficacy of treatment with trazodone in combination with pindolol or fluoxetine in major depression. J Affect Disord 141 (1996) 201-210
47. Mahesh R., Rajkumar R., Minasri B., and Venkatesha Perumal R. Potential antidepressants: pharmacology of 2-(4-methyl piperazin-1-yl)-1, 8-naphthyridine-3-carbonitrile in rodent behavioral models. Pharmazie 62 (2007) 919-924
48. Malick J.B., Doren E., and Barnett A. Quipazine-induced head-twitch in mice. Pharmacol Biochem Behav 6 (1977) 325-329
49. 2 and beta-adrenergic receptor binding in the frontal cortices of suicide victims. Arch Gen Psychiatry 43 (1986) 945-959
50. Mar A., Spreekmeester E., and Rochford J. Antidepressants preferentially enhance habituation to novelty in the olfactory bulbectomized rat. Psychopharmacology (Berl). 150 (2000) 52-60
51. 2A antagonists and selective serotonin reuptake inhibitors in neuropsychiatric disorders. Neuropsychopharmacology 28 (2003) 402-412
52. 2A antagonist (M100907) and the SSRI fluoxetine on DRL 72-s behavior. Abstr Soc Neurosci 27 (2001) 975-978
53. 2A receptor antagonist M100907 enhances antidepressant-like behavioral effects of the SSRI fluoxetine. Neuropsychopharmacology 30 (2005) 2205-2215
54. 2A receptors studied in depressive patients during chronic treatment by selective serotonin reuptake inhibitors. Psychopharmacology (Berl) 133 (1997) 99-101
55. 2H]harman binding experiments: I A reversible and selective radioligand for monoamine oxidase subtype A in the CNS of the rat. J Neurochem 56 (1991) 490-499
56. McDonald A.J., and Mascagni F. Neuronal localization of 5-HT type 2A receptor immunoreactivity in the rat basolateral amygdala. Neuroscience 146 (2007) 306-320
57. 2A receptor binding is reduced in drug-naive and unchanged in SSRI-responder depressed patients compared to healthy controls: a PET study. Psychopharmacology (Berl) 167 (2003) 72-78
58. 2A receptors in the middle layers of the rat prelimbic prefrontal cortex. Neuroscience 116 (2003) 107-117
59. Monleon S., D'Aquila P., Parra A., Simon V.M., Brain P.F., and Willner P. Attenuation of sucrose consumption in mice by chronic mild stress and its restoration by imipramine. Psychopharmacology (Berl). 117 (1995) 453-457
60. Montgomery S.A. Fast-onset antidepressants. Int Clin Psychopharmacol 12 (1997) S1-S5
61. 2A binding sites and their relationship to behaviour. Br J Pharmacol 117 (1996) 1481-1486
62. Muscat R., Sampson D., and Willner P. Dopaminergic mechanism of imipramine action in an animal model of depression. Biol Psychiatry 28 (1990) 223-230
63. Nacca A., Guiso G., Fracasso C., Cervo L., and Caccia S. Brain-to-blood partition and in vivo inhibition of 5-hydroxytryptamine reuptake and quipazine-mediated behaviour of nefazodone and its main active metabolites in rodents. Br J Pharmacol 125 (1998) 1617-1623
64. Nurimoto S., Ogawa N., and Ueki S. Effects of psychotropic drugs on hyper-emotionality of rats with bilateral ablations of the olfactory bulbs and olfactory tubercles. Jpn J Pharmacol 24 (1974) 185-193
65. O'Connor W.T., and Leonard B.E. Behavioural and neuropharmacological properties of the dibenzazepines, desipramine and lofepramine: studies on the olfactory bulbectomized rat model of depression. Prog Neuropsychopharmacol Biol Psychiatry 12 (1988) 41-51
66. Olivier B., Molewijk H.E., van der Heyden J.A., van Oorschot R., Ronken E., Mos J., et al. Ultrasonic vocalizations in rat pups: effects of serotonergic ligands. Neurosci Biobehav Rev 23 (1998) 215-227
67. O'Neill M.F., and Conway M.W. Role of 5-HT (1A) and 5-HT(1B) receptors in the mediation of behavior in the forced swim test in mice. Neuropsychopharmacology 24 (2001) 391-398
68. Ostroff R.B., and Nelson J.C. Risperidone augmentation of selective serotonin reuptake inhibitors in major depression. J Clin Psychiatry 60 (1999) 256-259
69. Pandey D.K., Rajkumar R., Mahesh R., and Radha R. Depressant-like effects of parthenolide in rodent behavioral anti-depressant test battery. J Pharm Pharmacol 60 (2008) 1643-1650
70. Papakostas G.I., and Fava M. A meta-analysis of clinical trials comparing the serotonin (5HT)-2 receptor antagonists trazodone and nefazodone with selective serotonin reuptake inhibitors for the treatment of major depressive disorder. Eur Psychiatry 22 (2007) 444-447
71. Papakostas G.I., Homberger C.H., and Fava M. A meta-analysis of clinical trials comparing mirtazapine with selective serotonin reuptake inhibitors for the treatment of major depressive disorder. J Psychopharmacol 22 (2008) 843-848
72. 2A receptor antagonist, EMD 281014, significantly increases swimming and decreases immobility in male congenital learned helpless rats in the forced swim test. Synapse 52 (2004) 73-75
73. Peroutka S.J., and Snyder S.H. Long-term antidepressant treatment decreases spiroperidol-labeled serotonin receptor binding. Science 210 (1980) 88-90
74. Porsolt R.D., Bertin A., and Jalfre M. "Behavioral despair" in rats and mice: strain differences and the effects of imipramine. Eur J Pharmacol 51 (1978) 291-294
75. Porsolt R.D., Bertin A., and Jalfre M. Behavioral despair in mice: a primary screening test for antidepressants. Arch Int Pharmacodyn Ther 229 (1977) 327-336
76. Pullar I.A., Carney S.L., Colvin E.M., Lucaites V.L., Nelson D.L., and Wedley S. LY367265, an inhibitor of the 5-hydroxytryptamine transporter and 5-hydroxytryptamine(2A) receptor antagonist: a comparison with the antidepressant, nefazodone. Eur J Pharmacol. 407 (2000) 39-46
77. Rajkumar R., Pandey D.K., Mahesh R., and Radha R. 1-(m-Chlorophenyl)piperazine induces depressogenic-like behaviour in rodents by stimulating the neuronal 5-HT(2A) receptors: proposal of a modified rodent antidepressant assay. Eur J Pharmacol 608 (2009) 32-41
78. Ramamoorthy R., Radhakrishnan M., and Borah M. Antidepressant-like effects of serotonin type-3 antagonist, ondansetron: an investigation in behavior-based rodent models. Behav Pharmacol 19 (2008) 29-40
79. Rasmussen K. Creating more effective antidepressants: clues from the clinic. Drug Discov Today 11 (2006) 623-631
80. 3 receptors in the activity of antidepressants in the mouse forced swimming test. Eur J Pharmacol 325 (1997) 129-135
81. 2A-mediated neurotransmission in BDNF conditional mutant mice. J Neurobiol 66 (2006) 408-420
82. Rodrigues A.L., da Silva G.L., Mateussi A.S., Fernandes E.S., Miguel O.G., Yunes R.A., et al. Involvement of monoaminergic system in the antidepressant-like effect of the hydroalcoholic extract of Siphocam-pylus verticillatus. Life Sci 70 (2002) 1347-1358
83. Rommelspacher H., May T., and Salewski B. Harman (1-methylbeta-carboline) is a natural inhibitor of monoamine oxydase type A in rats. Eur J Pharmacol 252 (1994) 51-59
84. 3 and cAMP in brains from depressed violent suicide victims. Neuropsychobiology 49 (2004) 189-195
85. Sällström-Baum S., Hill R., and Rommelspacher H. Harman induced changes of extracellular concentrations of neurotransmitters in the nucleus accumbens of rats. Eur J Pharmacol 314 (1996) 75-82
86. Schreiber R., Brocco M., Audinot V., Gobert A., Veiga S., and Millan M.J. 1-(2, 5-dimethoxy-4 iodophenyl)-2-aminopropane)-induced head-twitches in the rat are mediated by 5-hydroxytryptamine (5-HT) 2A receptors: modulation by novel 5-HT2A/2C antagonists, D1 antagonists and 5-HT1A agonists. J Pharmacol Exp Ther 273 (1995) 101-112
87. 2A receptors in postmortem prefrontal cortex in major depression is associated with reduced activity of protein kinase A. Neuroscience 158 (2009) 1406-1415
88. Shelton R.C., Tollefson G.D., Tohen M., Stahl S., Gannon K.S., Jacobs T.G., et al. A novel augmentation strategy for treating resistant major depression. Am J Psychiatry 158 (2001) 131-134
89. Shibata S., Nakanishi H., Watanabe S., and Ueki S. Effects of chronic administration of antidepressants on mouse-killing behavior (muricide) in olfactory bulbectomized rats. Pharmacol Biochem Behav 21 (1984) 225-230
90. Sibille E., Sarnyai Z., Benjamin D., Gal J., Baker H., and Toth M. Antisense inhibition of 5-hydroxytryptamine2a receptor induces an antidepressant-like effect in mice. Mol Pharmacol 52 (1997) 1056-1063
91. 3 receptors. Psychopharmacology (Berl) 175 (2004) 163-169
92. Smeraldi A., Aguglia M., Cattaneo C., Cerati C., Covelli M., Del Zompo C., et al. Double-blind, randomized study of venlafaxine, clomipramine, and trazodone in geriatric patients with major depression. Eur Neuropsychopharmacol 7 (1997) S170
93. Song C., and Leonard B.E. The olfactory bulbectomized rat as a model of depression. Neurosci Biobehav Rev 29 (2005) 627-647
94. Stahl S.M. Mood disorders. In: Stahl S.M. (Ed). Stahl's essential psychopharmacology: neuroscientific basis and practical applications (2008), Cambridge University Press 511-666
95. Stanley M., and Mann J.J. Increased serotonin-2 binding sites in frontal cortex of suicide victims. Lancet 1 (1983) 214-216
96. Steru L., Chermat R., Thierry B., and Simon P. The tail suspension test: a new method for screening antidepressant drugs. Psychopharmacology (Berl) 85 (1985) 367-370
97. Szabo S.T., and Blier P. Effects of serotonin (5-hydroxytryptamine, 5-HT) reuptake inhibition plus 5-HT(2A) receptor antagonism on the firing activity of norepinephrine neurons. J Pharmacol Exp Ther 302 (2002) 983-991
98. Taylor D.P., Carter R.B., Eison A.S., Mullins U.L., Smith H.L., Torrente J.R., et al. Pharmacology and neurochemistry of nefazodone, a novel antidepressant drug. J Clin Psychiatry 56 (1995) 3-11
99. Ter Laak A.M., Tsai R.S., Donné-Op den Kelder G.M., Carrupt P.A., Testa B., and Timmerman H. Lipophilicity and hydrogen-bonding capacity of H1-antihistaminic agents in relation to their central sedative side-effects. Eur J Pharm Sci 2 (1994) 373-384
100. Ulug B., Özerdem A., Oral E.T., Karaagaoglu E., and Gögüs A. Nefazodone in the treatment of depression: efficacy and tolerability data from a prospective open clinical trial. Eur Neuropsychopharmacol 11 (2001) S189
101. 2A receptor-mediated regulation of brain-derived neurotrophic factor mRNA in the hippocampus and the neocortex. J Neurosci 17 (1997) 2785-2795
102. 2A receptors in the stress-induced down-regulation of brain-derived neurotrophic factor expression in rat hippocampus. Neurosci Lett 262 (1999) 1-4
103. van Oekelen D., Jurzak M., van de Wiel D., van Hecke G., Luyten W.H., and Leysen J.E. Different regulation of rat 5-HT(2A) and rat 5-HT(2C) receptors in NIH 3 T3 cells upon exposure to 5-HT and pipamperone. Eur J Pharmacol 425 (2001) 21-32
104. 2C receptors and their atypical regulation properties. Life Sci. 72 (2003) 2429-2449
105. van Riezen H., and Leonard B.E. Effects of psychotropic drugs on the behavior and neurochemistry of olfactory bulbectomised rats. Pharmacol Ther 47 (1990) 21-34
106. Wang D., Yukihiro N., Hiroko T., and Zhou Y. Behavioral and neurochemical features of olfactory bulbectomized rats resembling depression with comorbid anxiety. Behav Brain Res 178 (2007) 262-273
107. Wang SH., Zhang Z., Guo Y., Zhou H., Teng G., and Chen B. Anhedonia and activity deficits in rats: impact of post-stroke depression. J Psychopharmacol 23 (2009) 295-304
108. Willner P., Towell A., and Sampson D. Reduction of sucrose preference by chronic unpredictable mild stress, and its restoration by a tricyclic antidepressant. Psychopharmacology (Berl) 93 (1987) 358-364
109. Willner P. Animal models of depression: an overview. Pharmacol Ther 45 (1990) 425-454
110. Willner P. The mesolimbic dopamine system as a target for rapid antidepressant action. Int Clin Psychopharmacol 12 (1997) S7-S14
111. Xu T., and Pandey S.C. Cellular localization of serotonin(2A) (5HT(2A)) receptors in the rat brain. Brain Res Bull 51 (2000) 499-505
112. Xu Y., Ku B.S., Yao H.Y., Lin Y.H., Ma X., Zhang Y.H., et al. Antidepressant effects of curcumin in the forced swim test and olfactory bulbectomy models of depression in rats. Pharmacol Biochem Behav 82 (2005) 200-206
113. 2A receptor function by chronic administration of selective serotonin reuptake inhibitors. Brain Res 1067 (2006) 164-169
114. 2 receptor changes in major depression. Biol Psychiatry 27 (1990) 489-496
115. Yatham L.N., and Steiner M. Neuroendocrine probes of serotonergic function: a critical review. Life Sci 53 (1993) 447-463